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P450

Cytochrome P450 are a family of heme-containing monoxygenases catalyzing the metabolism of xenobiotics in the body where P450 enzymes use O2 and two electrons provided by NAD(P)H with the help of redox partner flavoproteins and iron-sulfur proteins to catalyze the monooxygenation of a variety of substrates. Based on how electrons from NAD(P)H are delivered to the catalytic site, P450 enzymes are divided into four classes, including Class I requiring both an FAD-containing reductase and an iron sulfur redoxin, Class II requiring only an FAD/FMN-containg P450 reductase, Class III requiring no electron donor and Class IV requiring electrons directly from NAD(P)H.

  1. Cat.No. 产品名称 Information
  2. GC67933 LKY-047 LKY-047,是 Decursin 的一种衍生物,是一种有效的选择性的可逆竞争性的细胞色素 P45022J2 (CYP2J2) 抑制剂,IC50 为 1.7 μM。LKY-047 对其他人类 P450 无效,例如 CYP1A2、CYP2A6、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6、CYP2E1 和 CYP3A。
  3. GC66197 α-?Terpinyl acetate α-Terpinyl acetate 是从 Laurus nobilis L. 精油中分离出的一种单萜酯。α-Terpinyl acetate 是竞争性的 P450 2B6 底物,与其活性部位结合的 Kd 值为 5.4 ?μM 。
  4. GC52132 N-desmethyl Diltiazem (hydrochloride) An active metabolite of diltiazem
  5. GC65517 4-(Trifluoromethyl)umbelliferone 4-(Trifluoromethyl)umbelliferone 是大鼠肝细胞色素 P450 酶的荧光探针底物。
  6. GC65345 BI 653048 BI 653048 是一种选择性且口服的非甾体类糖皮质激素 (glucocorticoid (GC)) 激动剂,其 IC50 值为 55 nM。BI 653048 抑制 CP1A2,CYP2D6,CYP2C9,CYP2C19 和 CYP3A4 的活性并降低对 hERG 离子通道的亲和力 (IC50>30 μM)。BI 653048 源于专利 WO2005028501A1 (化合物 103),它也是一种 HCV NS3 protease 抑制剂,可以减少感染丙型肝炎病毒的病毒载量。
  7. GC65260 EDP-305 EDP-305 是一种口服有效且选择性的 farnesoid X 受体 (FXR) 激动剂,其 EC50 值为 34 nM (CHO 细胞嵌合性 FXR) 和 8 nM (HEK 细胞全长 FXR)。EDP-305 显示出强大而持久的抗纤维化作用。EDP-305 可用于原发性胆道胆管炎 (PBC) 和非酒精性脂肪性肝炎 (NASH) 研究。
  8. GC65088 Atovaquone-d5 Atovaquone-d5 (Atavaquone-d5) 是 Atovaquone 的氘代物。Atovaquone (Atavaquone) 是一种有效的、具有口服活性的选择性寄生虫线粒体细胞色素 bc1 (parasite's mitochondrial cytochrome bc1) 复合物的抑制剂。Atovaquone 抑制人类和 P. falciparum 细胞色素 bc1 活性,IC50 值分别为 460 nM 和 2.0 nM。Atovaquone 是一种抗疟 (antimalarial agent) 试剂,有潜力用于肺孢子虫肺炎、弓形体病、疟疾和巴贝斯虫病的相关研究。
  9. GC52083 21-Deoxycortisone A corticosteroid metabolite of 11-keto progesterone
  10. GC52062 7-Benzyloxy-4-(trifluoromethyl)coumarin A fluorogenic substrate for CYP1A2 and CYP3A
  11. GC52060 Trimipramine N-oxide Trimipramine N-oxide 是三环抗抑郁药 trimipramine 的活性代谢物。
  12. GC52045 N-desmethyl Azelastine N-去甲基氮卓斯汀是氮卓斯汀的主要活性代谢物,经细胞色素P450酶系统氧化代谢,蛋白结合率为97%,消除半衰期为54小时。
  13. GC52038 Desthiazolylmethyl Ritonavir A ritonavir degradation product
  14. GC52024 Aripiprazole N-oxide A metabolite of aripiprazole
  15. GC52019 Norpropranolol (hydrochloride) An active metabolite of propranolol
  16. GC52007 N-hydroxylamine Dapsone An active metabolite of dapsone
  17. GC49875 (±)-N-desmethyl Venlafaxine (hydrochloride) A minor active metabolite of venlafaxine
  18. GC49866 Desmethyl Carvedilol An active metabolite of carvedilol
  19. GC49855 Harmalol (hydrochloride hydrate) A β-carboline alkaloid and an active metabolite of harmaline
  20. GC49851 Norquetiapine An active metabolite of quetiapine
  21. GC49842 Digoxigenin Bisdigitoxoside A Na+/K+-ATPase inhibitor
  22. GC49832 Hydroxymetronidazole 羟基甲硝唑 (Metronidazole-OH) 是甲硝唑的代谢物,属于硝基咪唑类。
  23. GC49817 Desethoxy Quetiapine (hydrochloride) An active metabolite of quetiapine
  24. GC64010 Abiraterone decanoate Abiraterone decanoate 是一种有效的 Abiraterone 前药。Abiraterone decanoate 通过肌肉内 (IM) 递送提供 Abiraterone 的受控释放和长效 CYP17 抑制。
  25. GC63872 Dagrocorat hydrochloride Dagrocorat (PF-00251802) hydrochloride 是一种具有口服活性,选择性和高亲和性部分糖皮质激素受体的激动剂。Dagrocorat hydrochloride 也是一种时间依赖性可逆抑制剂,对 CYP3A (IC50=1.3 μM) 和CYP2D6 (Ki=0.57 μM) 有抑制作用。Dagrocorat hydrochloride 可用于类风湿性关节炎的研究。
  26. GC49686 N-desmethyl Regorafenib N-oxide An active metabolite of regorafenib
  27. GC49629 6β-hydroxy Prednisolone A metabolite of prednisolone
  28. GC49627 Rabeprazole sulfone A metabolite of rabeprazole
  29. GC49583 N-desmethyl Sertraline (hydrochloride) A metabolite of sertraline
  30. GC49559 Hydroxymethyl Tolperisone (hydrochloride) A metabolite of tolperisone
  31. GC49544 8-hydroxy Mirtazapine A metabolite of mirtazapine
  32. GC49503 Thujopsene A sesquiterpene with diverse biological activities
  33. GC49501 Nirvanol An active metabolite of mephenytoin
  34. GC63469 Abiraterone-D4 Abiraterone-D4 (CB-7598-D4) 是 Abiraterone 的氘代物。Abiraterone 是一种有效的不可逆的 CYP17A1 抑制剂,具有抗雄激素活性,抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶和 17,20-裂合酶活性,IC50 值 分别为 2.5 nM 和 15 nM.
  35. GC63272 β-Apo-8’-carotenal β-Apo-8’-carotenal (Apocarotenal) 是一种维生素原 A 类胡萝卜素,是大鼠CYP1A1 和 CYP1A2 的诱导剂。 β-Apo-8’-carotenal 存在于许多水果和蔬菜中。
  36. GC63199 Soticlestat A cholesterol 24-hydroxylase/CYP46A1 inhibitor
  37. GC49439 (±)11(12)-DiHET MaxSpec® Standard A quantitative analytical standard guaranteed to meet MaxSpec® identity, purity, stability, and concentration specifications
  38. GC49429 6-keto Lithocholic Acid 石胆酸的代谢产物
  39. GC49421 Atorvastatin lactone-d5 An internal standard for the quantification of atorvastatin lactone
  40. GC49410 CVT-2738 An active metabolite of ranolazine
  41. GC49409 Desmethyl Ranolazine A metabolite of ranolazine
  42. GC49403 Benzarone Benzarone (Fragivix) 是一种有效的人类尿酸转运蛋白 1 (hURAT1) 抑制剂,在卵母细胞中的 IC50 为 2.8 μM。
  43. GC49399 N-Desbutyl Dronedarone (hydrochloride) 决奈达隆的主要代谢物 Debutyldronedarone (SR35021) hydrochloride 是一种选择性甲状腺激素受体 α1 (TRα1) 抑制剂。
  44. GC49362 2-Amino-3,8-dimethylimidazo-[4,5-f]-quinoxaline A food-derived carcinogen
  45. GC49355 Norfluoxetine-d5 (hydrochloride) An internal standard for the quantification of norfluoxetine
  46. GC49320 7-Ethoxy-4-(trifluoromethyl)coumarin 7-Ethoxy-4-(trifluoromethyl)coumarin 是细胞色素 P450 超家族各种酶的荧光底物
  47. GC49291 rac-N-desmethyl Ivabradine-d6 (hydrochloride) An internal standard for the quantification of N-desmethyl ivabradine
  48. GC49288 Dolutegravir M1 A metabolite of dolutegravir
  49. GC49281 SPA70 SPA70 是一种有效的选择性人孕烷 X 受体 (hPXR) 拮抗剂,IC50 为 540 nM (Ki=390 nM)。 SPA70可以增强癌细胞的化学敏感性。
  50. GC49230 Ferroprotoporphyrin Ferroprotoporphyrin 是亚铁和卟啉的复合物,是脂肪酸与大鼠肝脏脂肪酸结合蛋白结合的等排抑制剂。
  51. GC49212 trans-carboxy Glimepiride A metabolite of glimepiride

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